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化合物简介
Tinzaparin is an antithrombotic drug in the heparin group. It is a low molecular weight heparin (LMWH) marketed as Innohep worldwide. It has been approved by the U.S. Food and Drug Administration (FDA) for once daily treatment and prophylaxis of deep vein thrombosis and pulmonary embolism. Tinzaparin sodium is the only low molecular weight heparin shown to be safe in pregnancy and in critically ill people with renal failure at both treatment and prophylaxis dose levels.
基本信息
CAS:9005-49-6
中文别名:
英文别名:thrombophob;HED heparin;clarin;Enoxaparine;liquaemin;pularin;Depo heparin;
分子式:C26H42N2O37S5
分子量:1134.93
精确质量:1134.01
Psa:652.39
Logp:-4.5261
中文别名:
英文别名:thrombophob;HED heparin;clarin;Enoxaparine;liquaemin;pularin;Depo heparin;
分子式:C26H42N2O37S5
分子量:1134.93
精确质量:1134.01
Psa:652.39
Logp:-4.5261
编号系统
EINECS号:232-681-7
物化性质
外观与性状:白色或类白色结晶粉末
密度:2.18 g/cm3
沸点:644.9ºC at 760mmHg
闪点:343.8ºC
折射率:1.711
稳定性:Hygroscopic; ampuled solution may be stored at room temperature for at least 12 mo sodium salt.
储存条件:Keep in a cool, dry, dark location in a tightly sealed container or cylinder. Keep away from incompatible materials, ignition sources and untrained individuals. Secure and label area. Protect containers/cylinders from physical damage.
密度:2.18 g/cm3
沸点:644.9ºC at 760mmHg
闪点:343.8ºC
折射率:1.711
稳定性:Hygroscopic; ampuled solution may be stored at room temperature for at least 12 mo sodium salt.
储存条件:Keep in a cool, dry, dark location in a tightly sealed container or cylinder. Keep away from incompatible materials, ignition sources and untrained individuals. Secure and label area. Protect containers/cylinders from physical damage.
安全信息
RTECS号:MI0850000
安全说明:S24/25
WGK Germany:2
海关编码:3001901000
安全说明:S24/25
WGK Germany:2
海关编码:3001901000
生产方法及用途
生产方法
方法一、酶解-树脂法酶解 取100kg新鲜肠黏膜(总固体5%-7%),加苯酚200ml (0.2%),如气温低时可不加。在搅拌下加入绞碎胰0.5-1kg(0.5%-1%),用 300-400g/L(30%-40%)NaOH溶液调节pH8.5-9,升温至40-45℃,保温2-3h。pH8,再加5kg粗食盐(5%)升温至90℃左右,用6mol/L HCl调节pH 6.5左右,停止搅拌,保温20min,以布袋过滤,得酶解滤液。肠黏膜[胰浆,NaOH]→[pH8.5-9, 40-45℃, 保温2-3h]肠黏膜液[NaCl, 6mol/L HCl]→[pH8; 90℃, pH6.5]滤液吸附、洗涤、洗脱 取上述滤液冷至50℃以下,用6mol/L NaOH调节pH7,加入5kgD-254强碱性阴离子交换树脂,搅拌5h左右,交换完毕,弃去液体,用自来水漂洗树脂至水清,用与树脂等体积的2mol/L NaCl,搅拌洗涤15min,弃去洗涤液,再加2倍树脂体积的1.2mol/L NaCl洗涤2次。用约树脂体积一半的5mol/L NaCl洗脱1h,收集洗脱液,然后用约树脂体积的1/3的3mol/L NaCl洗脱2次,合并洗脱液。滤液[D-254树脂, NaOH]→[pH7, 5h]吸附物[NaCl]→[2mol/L→1.2mol/L, →5mol/L, →3mol/L]洗脱液沉淀、脱水、干燥 将洗脱液用滤纸浆助滤,过滤1次,澄清滤液以体积计加入用活性炭处理过的0.9倍的95%乙醇,冷处沉淀8-12h。虹吸上清液弃去,按100kg黏膜加300ml的比例向沉淀中补加蒸馏水,再加入4倍量95%乙醇,冷处放置6h,收集沉淀,用无水乙醇脱水1次,丙酮脱水2次,置P2O5干燥器中真空干燥,得肝素钠粗品。洗脱液 → 沉淀物[无水乙醇;丙酮]→[P2O5]肝素钠粗品脱色、沉淀、干燥 用20g/L(2%)氯化钠溶液配成10 该品是制抗凝药肝素剂的原料。
用途
该品是制抗凝药肝素剂的原料。
方法一、酶解-树脂法酶解 取100kg新鲜肠黏膜(总固体5%-7%),加苯酚200ml (0.2%),如气温低时可不加。在搅拌下加入绞碎胰0.5-1kg(0.5%-1%),用 300-400g/L(30%-40%)NaOH溶液调节pH8.5-9,升温至40-45℃,保温2-3h。pH8,再加5kg粗食盐(5%)升温至90℃左右,用6mol/L HCl调节pH 6.5左右,停止搅拌,保温20min,以布袋过滤,得酶解滤液。肠黏膜[胰浆,NaOH]→[pH8.5-9, 40-45℃, 保温2-3h]肠黏膜液[NaCl, 6mol/L HCl]→[pH8; 90℃, pH6.5]滤液吸附、洗涤、洗脱 取上述滤液冷至50℃以下,用6mol/L NaOH调节pH7,加入5kgD-254强碱性阴离子交换树脂,搅拌5h左右,交换完毕,弃去液体,用自来水漂洗树脂至水清,用与树脂等体积的2mol/L NaCl,搅拌洗涤15min,弃去洗涤液,再加2倍树脂体积的1.2mol/L NaCl洗涤2次。用约树脂体积一半的5mol/L NaCl洗脱1h,收集洗脱液,然后用约树脂体积的1/3的3mol/L NaCl洗脱2次,合并洗脱液。滤液[D-254树脂, NaOH]→[pH7, 5h]吸附物[NaCl]→[2mol/L→1.2mol/L, →5mol/L, →3mol/L]洗脱液沉淀、脱水、干燥 将洗脱液用滤纸浆助滤,过滤1次,澄清滤液以体积计加入用活性炭处理过的0.9倍的95%乙醇,冷处沉淀8-12h。虹吸上清液弃去,按100kg黏膜加300ml的比例向沉淀中补加蒸馏水,再加入4倍量95%乙醇,冷处放置6h,收集沉淀,用无水乙醇脱水1次,丙酮脱水2次,置P2O5干燥器中真空干燥,得肝素钠粗品。洗脱液 → 沉淀物[无水乙醇;丙酮]→[P2O5]肝素钠粗品脱色、沉淀、干燥 用20g/L(2%)氯化钠溶液配成10 该品是制抗凝药肝素剂的原料。
用途
该品是制抗凝药肝素剂的原料。